1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR
  3. Tucatinib

Tucatinib (Synonyms: Irbinitinib; ARRY-380; ONT-380)

Cat. No.: HY-16069 Purity: 99.82%
Handling Instructions

Tucatinib (Irbinitinib; ARRY-380; ONT-380) is a potent and selective HER2 inhibitor with an IC50 of 8 nM.

For research use only. We do not sell to patients.

Tucatinib Chemical Structure

Tucatinib Chemical Structure

CAS No. : 937263-43-9

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10 mM * 1 mL in DMSO USD 99 In-stock
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50 mg USD 250 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Tucatinib (Irbinitinib; ARRY-380; ONT-380) is a potent and selective HER2 inhibitor with an IC50 of 8 nM.

IC50 & Target

HER2

 

In Vitro

Tucatinib (ONT-380) is a potent, selective, ATP-competitive, orally administered small-molecule inhibitor of HER2. Tucatinib has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR. In HER2 overexpressing cell lines, Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt. By contrast, in the EGFR overexpressing cell lines, it weakly inhibits phosphorylation and proliferation, demonstrating that Tucatinib may have potential to block HER2 signaling without causing the toxicities of EGFR inhibition[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In preclinical studies with intracranial tumor models, treatment of mice with Tucatinib (ONT-380) compared with GW572016 or neratinib shows a survival benefit when each drug is dosed at the maximum-tolerated dose[1]. In the Tucatinib (ARRY-380)-treated-group, 75% of the animals are alive on Day 43. Tucatinib and its active metabolite causes a significant reduction in brain pErbB2 (80%)[2]. Tucatinib (ARRY-380) demonstrates significant dose-related tumor growth inhibition (TGI; 50% at 50 mg/kg/d and 96% at 100 mg/kg/d) with numerous partial regressions (>50% reduction from baseline size) at the higher dose level in 9/12 animals. Tucatinib (50 mg/kg/d) in combination with trastuzumab shows a 98% TGI with complete regressions in 9/12 animals and two partial regressions. At dose of 100 mg/kg/d of Tucatinib in combination with trastuzumab, there is 100% TGI and all animals have complete responses[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

480.52

Formula

C₂₆H₂₄N₈O₂

CAS No.

937263-43-9

SMILES

CC1=CC(NC2=C3C=C(NC4=NC(C)(C)CO4)C=CC3=NC=N2)=CC=C1OC5=CC6=NC=NN6C=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (104.05 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0811 mL 10.4054 mL 20.8108 mL
5 mM 0.4162 mL 2.0811 mL 4.1622 mL
10 mM 0.2081 mL 1.0405 mL 2.0811 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (4.33 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.33 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.33 mM); Clear solution

  • 4.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.62 mg/mL (5.45 mM); Clear solution

  • 5.

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.62 mg/mL (5.45 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[3]

Mice: For the SKOV-3 tumor studies, female nude mice are inoculated with cells subcutaneously in the flank. Animals received: doses of Tucatinib ranging up to 200 mg/kg/d, PO; and/or Trastuzumab at 20 mg/kg, IP, Q3D or QW; and/or RP-56976 at 10 mg/kg, IV, Q3D; and/or Bevacizumab at 10 mg/kg, IP, Q4D x3. Tumor size is measured at regular intervals and subsets of animals are monitored for up to 90 days to determine tumor-free survival[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.82%

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Keywords:

TucatinibIrbinitinib ARRY-380 ONT-380ARRY380ARRY 380ARRY-380ONT380ONT 380ONT-380EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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Tucatinib
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